Table 2.
Selected clinical trials of Aurora kinases inhibitors
| Inhibitor | Chemical structure | Target, selectivity (IC50) | NCT number, phase, status | Cancer type | Ref. |
|---|---|---|---|---|---|
| MLN8237 |
|
AURKA (2 nM) | NCT01898078, Phase 1, Ongoing | Advanced Solid Tumors; Lymphoma | |
| NCT01045421, Phase 1/Phase 2, Completed | Nonhematological Malignancies | [95] | |||
| NCT01091428 Phase 1/Phase 2, Ongoing (Agent in combination with Paclitaxel) | Ovarian Carcinoma; Fallopian Tube Cancer; Peritoneal Cancer; Breast Carcinoma | ||||
| NCT01471964, Phase 1/Phase 2, Ongoing (Agent in combination with Erlotinib) | Metastatic or Recurrent Non-Small Cell Lung Cancer | ||||
| NCT02114229, Phase 2, Ongoing | Malignant Rhabdoid Tumor; Atypical Teratoid Rhabdoid Tumor | ||||
| NCT00962091, Phase 1, Completed | Advanced Solid Tumors | ||||
| NCT01512758, Phase 1, Completed | Adult East Asian Patients With Advanced Solid Tumors or Lymphomas | ||||
| NCT02109328, Phase 2, Ongoing | Bladder Cancer; Transitional Cell Carcinoma | ||||
| NCT01812005, Phase 2, Ongoing (Agent in combination with Rituximab) | Relapsed or Refractory B-Cell Non-Hodgkin Lymphoma | ||||
| NCT01397825, Phase 1/Phase 2, Ongoing (Agent in combination with Rituximab and Vincristine) | Relapsed or Refractory Aggressive B-Cell Lymphoma | ||||
| NCT00500903, Phase 1, Completed | Advanced Solid Tumors | ||||
| NCT00697346, Phase 1, Completed | Advanced Hematological Malignancies | [110] | |||
| NCT01799278, Phase 2, Ongoing | Metastatic Castrate Resistant and Neuroendocrine Prostate Cancer | ||||
| NCT00807495, Phase 2, Completed | Aggressive Non-Hodgkin’s Lymphoma | ||||
| NCT01567709, Phase 1, Ongoing (Agent in combination with Vorinostat) | Relapsed or Recurrent Hodgkin Lymphoma, B-Cell Non-Hodgkin Lymphoma, or Peripheral T-Cell Lymphoma | ||||
| NCT00651664, Phase 1, Completed. | Advanced Solid Tumors; Lymphomas | ||||
| NCT01695941, Phase 1, Ongoing (Agent in combination with Bortezomib and Rituximab) | Relapsed or Refractory Mantle Cell Lymphoma or B-Cell Low Grade Non-Hodgkin Lymphoma | ||||
| NCT01154816, Phase 2, Completed | Recurrent or Refractory Solid Tumors or Leukemia | ||||
| NCT02038647, Phase 2, Ongoing (Agent in combination with Placebo and Paclitaxel) | Small Cell Lung Cancer | ||||
| NCT01779843, Phase 1, Ongoing (Agent in combination with Cytarabine and Idarubicin) | Acute Myeloid Leukemia | ||||
| NCT00830518, Phase 2, Completed | Acute Myelogenous Leukemia and High-Grade Myelodysplastic Syndrome | ||||
| NCT01677559, Phase 1, Ongoing (Agent in combination with Nab-Paclitaxel) | Advanced Solid Malignancies | ||||
| NCT01924260, Phase 1, Ongoing (Agent in combination with Gemcitabine) | Solid Tumors or Pancreatic Cancer | ||||
| NCT01897012, Phase 1, Ongoing (Agent in combination with Romidepsin) | Relapsed or Refractory B-Cell or T-Cell Lymphomas | ||||
| NCT01034553, Phase 1/Phase 2, Ongoing (Agent in combination with Bortezomib) | Relapsed or Refractory Multiple Myeloma | ||||
| NCT01482962, Phase 3, Ongoing (Agent in combination with Pralatrexate, Gemcitabine and Romidepsin) | Relapsed/Refractory Peripheral T-Cell Lymphoma | ||||
| NCT01848067, Phase 1/Phase 2, Ongoing (Agent in combination with Abiraterone acetate and Prednisone) | Hormone-Resistant Prostate Cancer | ||||
| NCT01466881, Phase 2, Ongoing | Relapsed or Refractory Peripheral T-Cell Non-Hodgkin Lymphoma | ||||
| NCT01923337, Phase 1, Ongoing (Agent in combination with Irinotecan hydrochloride) | Advanced Solid Tumors or Colorectal Cancer | ||||
| NCT01714947, Phase 1, Completed | Advanced Solid Tumors; Lymphoma | ||||
| NCT01094288, Phase 1, Ongoing (Agent in combination with Docetaxel) | Advanced Solid Tumors Including Castration-Resistant Prostate Cancer | ||||
| NCT01639911, Phase 1, Ongoing (Agent in combination with Pazopanib) | Solid Tumors | ||||
| NCT00853307, Phase 2, Completed | Ovarian, Fallopian Tube, or Peritoneal Carcinoma | ||||
| NCT01540682, Phase 1, Completed (Agent in combination with Cetuximab and radiotherapy) | Head and Neck Cancer | ||||
| NCT01316692, Phase 2, Ongoing | Unresectable Stage III-IV Melanoma | ||||
| NCT02187991, Phase 2, Ongoing (Agent in combination with Paclitaxel) | Metastatic or Locally Recurrent Breast Cancer | ||||
| NCT02259010, Phase 1, Ongoing (Agent in combination with Itraconazole) | Advanced Solid Tumors or Relapsed/Refractory Lymphoma | ||||
| NCT02367352, Phase 1, Ongoing (Agent in combination with Paclitaxel) | East Asian Patients With Advanced Solid Tumors | ||||
| NCT02319018, Phase 1, Ongoing (Agent in combination with Leucovorin Calcium, Fluorouracil, and Oxaliplatin) | Gastrointestinal Tumors | ||||
| NCT02219789, Phase 1, Ongoing (Agent in combination with Fulvestrant) | Hormone Receptor Positive, Metastatic or Advanced Breast Cancer | ||||
| NCT02186509, Phase 1, Ongoing (Agent with radiation) | Recurrent High-Grade Gliomas | ||||
| NCT01848067, Phase 1&2, Ongoing (Agent with Abiraterone acetate and Prednisone) | Hormone-Resistant Prostate Cancer | ||||
| NCT01779843, Phase 1, Ongoing (Agent with Cytarabine and Idarubicin) | Acute Myeloid Leukemia | ||||
| NCT02327169, Phase 1, Ongoing (Agent with MLN2480, MLN0128, and Paclitaxel) | Advanced Nonhematologic Malignancies | ||||
| NCT00543387, Phase 1, Completed (Agent in combination with Docetaxel) | Advanced and/or Refractory Solid Tumors | ||||
| MK-5108 |
|
AURKA (0.046 nM) | NCT01914510, Phase 2. Ongoing | Ovarian Clear Cell Cancers | |
| ENMD-2076 |
|
AURKA (14 nM) | NCT01719744, Phase 2. Ongoing | Advanced/Metastatic Soft Tissue Sarcoma | |
| NCT00904787, Phase 1. Completed | Relapsed or Refractory Hematological Malignancies | ||||
| NCT01639248, Phase 2. Ongoing | Advanced and Metastatic Triple-Negative Breast Cancer | ||||
| NCT00806065, Phase 1. Completed | Multiple Myeloma | ||||
| NCT00658671, Phase 1. Completed | Advanced Cancer | [100] | |||
| NCT02234986, Phase 2, Ongoing | Advanced Fibrolamellar Carcinoma | ||||
| NCT01104675, Phase 2, Completed | Ovarian Cancer |